GNF362

GNF362

G649476-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC 50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC 50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+ -dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4]. In Vitro GNF362 (0-10 mM) blocks Ins (1,3,4,5) P4 production, enhances antigen receptor-driven Ca 2+ responses and lead to apoptosis of activated T cells in an Itpkb-dependent manner in lymphocytes. GNF362 augments SOC responses following antigen receptor cross-linking, with an EC 50 of 12 nM in primary B or T lymphocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GNF362 (orally administration; 6 or 20 mg/kg; twice daily; 21 days) shows minimal block in antibody production but shows significant inhibition of joint swelling at 6 mg/kg, reduces inflammatory cell infiltrate, joint damage, and proteoglycan loss at 20 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: A Lewis rat antigen-induced arthritis (rAIA) model Dosage: 6 or 20 mg/kg Administration: Orally administration; 6 or 20 mg/kg; twice daily; 21 days Result: Reduced knee swelling in both the 20mg/kg and 6mg/kg treatment groups of GNF362 by 47% and 34%, respectively. Form:Solid

GNF362 是一种选择性强效口服生物活性抑制剂，可抑制肌醇三磷酸激酶 B（Itpkb），其 IC 50 值为 9 nM。GNF362 还能抑制 Itpka 和 Itpkc，其 IC 50 值分别为 20 nM 和 19 nM。三磷酸肌醇 3'激酶

1003019-41-7

C22H21F3N6

426.44 g/mol

57999583

C[C@@H]1CN(CCN1C2=NC=C(C=C2)C(F)(F)F)CC3=C(NN=C3)C4=CC=C(C=C4)C#N

4-[4-[[(3R)-3-methyl-4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]methyl]-1H-pyrazol-5-yl]benzonitrile

1S/C22H21F3N6/c1-15-13-30(8-9-31(15)20-7-6-19(12-27-20)22(23,24)25)14-18-11-28-29-21(18)17-4-2-16(10-26)3-5-17/h2-7,11-12,15H,8-9,13-14H2,1H3,(H,28,29)/t15-/m1/s1

VNTCGXMLDSKOKN-OAHLLOKOSA-N

CC1CN(CCN1C2=NC=C(C=C2)C(F)(F)F)CC3=C(NN=C3)C4=CC=C(C=C4)C#N

57999583

DMSO : 100 mg/mL (234.50 mM; Need ultrasonic)